当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Improved synthesis and comparative analysis of the tool properties of new and existing D-ring modified (S)-blebbistatin analogs.

Improved synthesis and comparative analysis of the tool properties of new and existing D-ring modified (S)-blebbistatin analogs.

Abstract：

:(S)-Blebbistatin is a widely used research tool to study myosin II, an important regulator of many motility based diseases. Its potency is too low to be of clinical relevance, but identification of analogs with enhanced potency could deliver leads for targeted pharmacotherapeutics. This, however, requires a profound insight into the structure-activity relationship of the (S)-blebbistatin scaffold. Therefore, new D-ring modified (S)-blebbistatin derivatives were prepared to extend the existing small library of analogs. These molecules were obtained via an improved synthesis pathway and their myosin II inhibitory properties were evaluated in vitro. Finally, all new and known D-ring modified (S)-blebbistatin analogs were compared and the most potent ones underwent a screening of their physicochemical properties.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Verhasselt S,Roman BI,Bracke ME,Stevens CV

doi

10.1016/j.ejmech.2017.04.072

subject

Has Abstract

pub_date

2017-08-18 00:00:00

pages

85-103

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(17)30354-9

journal_volume

136

pub_type

杂志文章

相关文献

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY文献大全
  • Exploration of (S)-3-aminopyrrolidine as a potentially interesting scaffold for discovery of novel Abl and PI3K dual inhibitors.

    abstract：:Based on the literature-reported compensatory effect of PI3K on Abl inhibition and the improved preclinical effect of drug combination of Abl and PI3K inhibitors, a series of compounds bearing novel scaffold of (S)-3-aminopyrrolidine was identified as Abl and PI3K dual inhibitors through support vector machine screeni...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.01.020

    authors： Zhang C,Tan C,Zu X,Zhai X,Liu F,Chu B,Ma X,Chen Y,Gong P,Jiang Y

    更新日期：2011-04-01 00:00:00

  • (Arene)Ru(II) complexes of epidermal growth factor receptor inhibiting tyrphostins with enhanced selectivity and cytotoxicity in cancer cells.

    abstract：:Ru(eta6-arene) complexes of epidermal growth factor receptor (EGFR) inhibiting tyrphostins 1a and 1b were prepared, characterized and tested for DNA interaction and bioactivity in four human tumor cell lines. The intrinsic cytotoxicity and cell line selectivity of o-hydroxyanisol 1a was greatly enhanced in its Ru(eta6...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.01.040

    authors： Biersack B,Zoldakova M,Effenberger K,Schobert R

    更新日期：2010-05-01 00:00:00

  • Structural modifications in the distal, regulatory region of histamine H3 receptor antagonists leading to the identification of a potent anti-obesity agent.

    abstract：:A series of 4-pyridylpiperazine derivatives with varying regulatory region substituents proved to be potent histamine H3 receptor (H3R) ligands in the nanomolar concentration range. The most influential modification that affected the affinity toward the H3R appeared by introducing electron-withdrawing moieties into th...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.113041

    authors： Szczepańska K,Pockes S,Podlewska S,Höring C,Mika K,Latacz G,Bednarski M,Siwek A,Karcz T,Nagl M,Bresinsky M,Mönnich D,Seibel U,Kuder KJ,Kotańska M,Stark H,Elz S,Kieć-Kononowicz K

    更新日期：2020-11-24 00:00:00

  • Hydroxymethyl bioisosteres of phenolic GluN2B-selective NMDA receptor antagonists: Design, synthesis and pharmacological evaluation.

    abstract：:Antagonists addressing selectively NMDA receptors containing the GluN2B subunit are of particular interest for the treatment of various neurological disorders including neurodegenerative diseases. With the aim to bioisosterically replace the metabolically labile phenol of 7-amino-6,7,8,9-tetrahydro-5H-benzo[7]annulen-...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2017.12.054

    authors： Temme L,Frehland B,Schepmann D,Robaa D,Sippl W,Wünsch B

    更新日期：2018-01-20 00:00:00

  • Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT(1A) activity. Part 5.

    abstract：:A series of novel 4-aryl-pyrido[1,2-c]pyrimidine derivatives containing a 1-(2-quinoline)piperazine moiety was synthesized. The chemical structure of new compounds was confirmed by FT-IR, (1)H NMR, (13)C NMR and HRMS spectra as well as elemental analysis. Affinity of the novel pyrido[1,2-c]pyrimidine derivatives for 5...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2015.05.003

    authors： Gomółka A,Ciesielska A,Wróbel MZ,Chodkowski A,Kleps J,Dawidowski M,Siwek A,Wolak M,Stachowicz K,Sławińska A,Nowak G,Satała G,Bojarski AJ,Belka M,Ulenberg S,Bączek T,Skowronek P,Turło J,Herold F

    更新日期：2015-06-15 00:00:00

  • Design and synthesis of fluorescent ligands for the detection of cannabinoid type 2 receptor (CB2R).

    abstract：:The Cannabinoid 2 receptor, CB2R, belonging to the endocannabinoid system, ECS, is involved in the first steps of neurodegeneration and cancer evolution and progression and thus its modulation may be exploited in the therapeutic and diagnostic fields. However, CB2Rs distribution and signaling pathways in physiological...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112037

    authors： Spinelli F,Giampietro R,Stefanachi A,Riganti C,Kopecka J,Abatematteo FS,Leonetti F,Colabufo NA,Mangiatordi GF,Nicolotti O,Perrone MG,Brea J,Loza MI,Infantino V,Abate C,Contino M

    更新日期：2020-02-15 00:00:00

  • Chalcones: Unearthing their therapeutic possibility as monoamine oxidase B inhibitors.

    abstract：:In the last years the continuous efforts in the development of novel and effective inhibitors of human monoamine oxidases (hMAOs) promoted the discovery of new agents able to effectively and selectively bound one of the two isoforms (hMAO-A and hMAO-B). However, the parent chalcone scaffold still covers an important r...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2020.112650

    authors： Guglielmi P,Mathew B,Secci D,Carradori S

    更新日期：2020-11-01 00:00:00

  • Design, synthesis and evaluation of Ospemifene analogs as anti-breast cancer agents.

    abstract：:The synthesis of some novel Ospemifene derived analogs and their evaluation as anti-breast cancer agents against MCF-7 (ER-positive) and MDA-MB-231 (ER-negative) human breast cancer cell lines are described. Few of these analogs for instance, compounds 6, 7 and 8 are shown to be more effective than recent Selective Es...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.08.050

    authors： Kaur G,Mahajan MP,Pandey MK,Singh P,Ramisetti SR,Sharma AK

    更新日期：2014-10-30 00:00:00

  • Carboline- and phenothiazine-derivated heterocycles as potent SIGMA-1 protein ligands.

    abstract：:Sigma 1 receptors are associated with neurodegenerative and psychiatric disorders. These receptors, via their chaperoning functions that counteract endoplasmic reticulum stress and block neurodegeneration, may serve as a target for a new generation of antidepressants or neuroprotective agents. The involvement of these...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.10.053

    authors： Donnier-Maréchal M,Larchanché PE,Le Broc D,Furman C,Carato P,Melnyk P

    更新日期：2015-01-07 00:00:00

  • An insight into the biological activities of heterocyclic-fatty acid hybrid molecules.

    abstract：:Heterocyclic compounds are the interesting core structures for the development of new bioactive compounds. Fatty acids are derived from renewable raw materials and exhibit various biological activities. Several researchers are amalgamating these two bioactive components to yield bioactive hybrid molecules with some de...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2017.09.069

    authors： Venepally V,Reddy Jala RC

    更新日期：2017-12-01 00:00:00

  • Design, synthesis and biological evaluation of novel α-acyloxy carboxamides via Passerini reaction as caspase 3/7 activators.

    abstract：:Evasion of apoptosis is a hallmark of cancer. Caspases; the key executors of apoptotic cascade are attractive targets for selective induction of apoptosis in cancer cells. Within this approach, various caspase activators were introduced as lead anticancer agents. In the current study, a new series of multifunctional P...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2019.02.051

    authors： Salah Ayoup M,Wahby Y,Abdel-Hamid H,Ramadan ES,Teleb M,Abu-Serie MM,Noby A

    更新日期：2019-04-15 00:00:00

  • Synthesis, cytotoxicity and DNA-binding levels of new type binuclear platinum(II) complexes.

    abstract：:Six new type binuclear platinum(II) complexes (a-f) have been synthesized and characterized by elemental analysis, conductivity, thermal analysis, IR, UV, (1)H NMR and mass spectra techniques. The cytotoxicity of the complexes was tested by MTT and SRB assays. The cell cycle analysis and the levels of total platinum b...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2009.06.017

    authors： Zhang J,Li Y,Sun J,Li W,Gong Y,Zheng X,Cui J,Wang R,Wu J

    更新日期：2009-11-01 00:00:00

  • Synthesis, molecular docking and anti-mycobacterial evaluation of new imidazo[1,2-a]pyridine-2-carboxamide derivatives.

    abstract：:New anti-tubercular agents, imidazo[1,2-a]pyridine-2-carboxamide derivatives (5a-q) have been designed and synthesized. The structural considerations of the designed molecules were further supported by the docking study with a long-chain enoyl-acyl carrier protein reductase (InhA). The chemical structures of the new c...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.10.079

    authors： Jose G,Suresha Kumara TH,Nagendrappa G,Sowmya HB,Sriram D,Yogeeswari P,Sridevi JP,Guru Row TN,Hosamani AA,Sujan Ganapathy PS,Chandrika N,Narendra LV

    更新日期：2015-01-07 00:00:00

  • Salicylanilides as inhibitors of the protein tyrosine kinase epidermal growth factor receptor.

    abstract：:A pharmacophore model for ATP-competitive inhibitors interacting with the active site of the EGFR protein tyrosine kinase and a putative binding mode of 4-anilinoquinazoline suggest that a salicylic acid function could serve as the pharmacophore replacement of a pyrimidine ring. Superpositions by CAMM of salicylanilid...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2003.09.010

    authors： Liechti C,Séquin U,Bold G,Furet P,Meyer T,Traxler P

    更新日期：2004-01-01 00:00:00

  • Synthesis, spectral characterization and bio-analysis of some organotin(IV) complexes.

    abstract：:Five novel organotin(IV) derivatives have been synthesized by refluxing trimethyl, triethyl, tributyl, and triphenyl and tribenzyltin chloride with Schiff base derived from salicylaldehyde and adenine. These compounds were characterized by spectroscopic (IR, (1)H, (13)C, (119)Sn-NMR, (119m)Sn Mössbauer) techniques and...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2008.01.019

    authors： Rehman W,Baloch MK,Badshah A

    更新日期：2008-11-01 00:00:00

  • Design, synthesis and biological evaluation of novel potent STAT3 inhibitors based on BBI608 for cancer therapy.

    abstract：:Persistently activated signal transducer and activator of transcription 3 (STAT3) plays an important role in the development of multiple cancers, and therefore is a potential therapeutic target for cancer prevention. Herein, we report the rational design, synthesis, and biological evaluation of novel potent STAT3 inhi...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112428

    authors： Feng KR,Wang F,Shi XW,Tan YX,Zhao JY,Zhang JW,Li QH,Lin GQ,Gao D,Tian P

    更新日期：2020-09-01 00:00:00

  • Polymeric bile acid sequestrants: Review of design, in vitro binding activities, and hypocholesterolemic effects.

    abstract：:Polymeric bile acid sequestrants (BAS) have recently attracted much attention as lipid-lowering agents. These non-absorbable materials specifically bind bile acids (BAs) in the intestine, preventing bile acid (BA) reabsorption into the blood through enterohepatic circulation. Therefore, it is important to understand t...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章,评审

    doi：10.1016/j.ejmech.2017.12.015

    authors： Heřmánková E,Žák A,Poláková L,Hobzová R,Hromádka R,Širc J

    更新日期：2018-01-20 00:00:00

  • Discovery of phenylselenoether-hydantoin hybrids as ABCB1 efflux pump modulating agents with cytotoxic and antiproliferative actions in resistant T-lymphoma.

    abstract：:Multidrug resistance (MDR) in cancer cells is a crucial aspect to consider for a successful cancer therapy. P-gp/ABCB1, a member of ABC transporters, is involved in the main tumour MDR mechanism, responsible for the efflux of drugs and cytotoxic substances. Herein, we describe a discovery of potent selenium-containing...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2020.112435

    authors： Ali W,Spengler G,Kincses A,Nové M,Battistelli C,Latacz G,Starek M,Dąbrowska M,Honkisz-Orzechowska E,Romanelli A,Rasile MM,Szymańska E,Jacob C,Zwergel C,Handzlik J

    更新日期：2020-08-15 00:00:00

  • Spirostanols obtained by cyclization of pseudosaponin derivatives and comparison of anti-platelet agglutination activities of spirostanol glycosides.

    abstract：:Naturally occurring saponins 3 and 4 have a normal type F ring and alpha-arranged CH(3)-21 group. Treatments of pseudosaponin peracetates 18 and 19 derived from 3 and 4, respectively, with alcoholic KOH, followed by acidification with acetic acid, gave spirostanols 20 and 22 having iso type F rings as major products. ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/s0223-5234(00)00151-3

    authors： Tobari A,Teshima M,Koyanagi J,Kawase M,Miyamae H,Yoza K,Takasaki A,Nagamura Y,Saito S

    更新日期：2000-05-01 00:00:00

  • Synthesis and biological activity of novel N6-substituted and 2,N6-disubstituted adenine ribo- and 3'-C-methyl-ribonucleosides as antitumor agents.

    abstract：:A series of N6-aminopurine-9-β-D-ribonucleosides and ribose-modified 3'-C-methyl analogues substituted at N6-position with a small group like hydroxy, methoxy or amino group or at C2(N6) position have been synthesized and tested against a panel of human leukemia and carcinoma cell lines. N6-Hydrazino-9-β-D-ribofuranos...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.01.055

    authors： Cappellacci L,Petrelli R,Franchetti P,Vita P,Kusumanchi P,Kumar M,Jayaram HN,Zhou B,Yen Y,Grifantini M

    更新日期：2011-05-01 00:00:00

  • New synthesis of 3-(β-D-glucopyranosyl)-5-substituted-1,2,4-triazoles, nanomolar inhibitors of glycogen phosphorylase.

    abstract：:O-Perbenzoylated 5-(β-D-glucopyranosyl)tetrazole was reacted with N-benzyl carboximidoyl chlorides to give the corresponding 4-benzyl-3-(β-D-glucopyranosyl)-5-substituted-1,2,4-triazoles. Removal of the O-benzoyl and N-benzyl protecting groups by base catalysed transesterification and catalytic hydrogenation, respecti...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2014.02.041

    authors： Kun S,Bokor É,Varga G,Szőcs B,Páhi A,Czifrák K,Tóth M,Juhász L,Docsa T,Gergely P,Somsák L

    更新日期：2014-04-09 00:00:00

  • Design, synthesis and identification of silicon-containing HCV NS5A inhibitors with pan-genotype activity.

    abstract：:Modification of a HCV NS5A inhibitor, ombitasvir, led to the identification of 10d with improved pan-genotype NS5A inhibition and better pharmacokinetic properties. The key structural changes to ombitasvir include bioisosteric replacement of carbon with silicon atom. Compared with ombitasvir, the activity of anti-HCV ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2018.02.025

    authors： Liu B,Gai K,Qin H,Liu X,Cao Y,Lu Q,Lu D,Chen D,Shen H,Song W,Zhang Y,Wang X,Xu H,Zhang Y

    更新日期：2018-03-25 00:00:00

  • Combretastatin A-4 derived 5-(1-methyl-4-phenyl-imidazol-5-yl)indoles with superior cytotoxic and anti-vascular effects on chemoresistant cancer cells and tumors.

    abstract：:5-(1-Methyl-4-phenyl-imidazol-5-yl)indoles 5 were prepared and tested as analogs of the natural vascular-disrupting agent combretastatin A-4 (CA-4). The 3-bromo-4,5-dimethoxyphenyl derivative 5c was far more active than CA-4 with low nanomolar IC50 concentrations against multidrug-resistant KB-V1/Vbl cervix and MCF-7/...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.04.045

    authors： Mahal K,Biersack B,Schruefer S,Resch M,Ficner R,Schobert R,Mueller T

    更新日期：2016-08-08 00:00:00

  • Novel pyrazolopyridine derivatives as potential angiogenesis inhibitors: Synthesis, biological evaluation and transcriptome-based mechanistic analysis.

    abstract：:Modified purine derivatives exemplified by pyrazolopyrimidines have emerged as highly selective inhibitors of several angiogenic receptor tyrosine kinases. Herein, we designed and synthesized a new series of substituted pyrazolopyridines and explored their ability to influence crucial pro-angiogenic attributes of endo...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.05.035

    authors： Michailidou M,Giannouli V,Kotsikoris V,Papadodima O,Kontogianni G,Kostakis IK,Lougiakis N,Chatziioannou A,Kolisis FN,Marakos P,Pouli N,Loutrari H

    更新日期：2016-10-04 00:00:00

  • New small 99mTc-labeled peptides for HER2 receptor imaging.

    abstract：:The high expression of the human epidermal growth factor receptor 2 (HER2) and the accessibility of its extracellular domain make it an ideal target for the targeted delivery of anti-tumor drugs as well as imaging agents. In this study, the heptapeptide leucine-threonine-valine-serine-proline-tryptophan-tyrosine (LTVS...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.11.011

    authors： Sabahnoo H,Noaparast Z,Abedi SM,Hosseinimehr SJ

    更新日期：2017-02-15 00:00:00

  • Urea/thiourea derivatives of quinazolinone-lysine conjugates: synthesis and structure-activity relationships of a new series of antimicrobials.

    abstract：:Synthesis of a series of urea/thiourea/acetamide/sulphonamide derivatives of quinazolinones conjugated lysine has been reported. Structures of the products have been determined by standard spectroscopical studies. All the compounds have been screened for their antibacterial studies and structure-activity relationship ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2011.03.041

    authors： Suresha GP,Suhas R,Kapfo W,Gowda DC

    更新日期：2011-06-01 00:00:00

  • Influence of enantiomers of 1-naphthylalanine in position 2 of VAVP and dVAVP on their pharmacological properties.

    abstract：:In this study, we described the synthesis and some pharmacological properties of four new analogues of arginine vasopressin (AVP). Two peptides are substituted in position 2 with L-1-naphthylalanine (L-1-Nal) or its D-enantiomer and in position 4 with valine. In the further two compounds, we combined the above modific...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2004.09.011

    authors： Derdowska I,Prahl A,Kowalczyk W,Janecki M,Melhem S,Trzeciak HI,Lammek B

    更新日期：2005-01-01 00:00:00

  • Synthesis, antiarrhythmic activity, and toxicological evaluation of mexiletine analogues.

    abstract：:Four mexiletine analogues have been tested for their antiarrhythmic, inotropic, and chronotropic effects on isolated guinea pig heart tissues and to assess calcium antagonist activity, in comparison with the parent compound mexiletine. All analogues showed from moderate to high antiarrhythmic activity. In particular, ...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.05.046

    authors： Roselli M,Carocci A,Budriesi R,Micucci M,Toma M,Di Cesare Mannelli L,Lovece A,Catalano A,Cavalluzzi MM,Bruno C,De Palma A,Contino M,Perrone MG,Colabufo NA,Chiarini A,Franchini C,Ghelardini C,Habtemariam S,Lentini G

    更新日期：2016-10-04 00:00:00

  • A molecular model for cocaine binding by the immunotherapeutic human/mouse chimeric monoclonal antibody 2E2.

    abstract：:Immunotherapy by cocaine-binding monoclonal antibodies (mAbs) has emerged as a promising strategy for the treatment of cocaine addiction. The human (gamma1 heavy chain)/murine (lambda light chain) chimeric mAb 2E2 has excellent affinity and specificity for cocaine and recent animal studies have demonstrated 2E2's abil...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2010.02.004

    authors： Lape M,Paula S,Ball WJ Jr

    更新日期：2010-06-01 00:00:00

  • The design of 8-hydroxyquinoline tetracyclic lactams as HIV-1 integrase strand transfer inhibitors.

    abstract：:A novel series of HIV-1 integrase strand transfer inhibitors were designed using the venerable two-metal binding pharmacophore model and incorporating structural elements from two different literature scaffolds. This manuscript describes a number of 8-hydroxyquinoline tetracyclic lactams with exceptional antiviral act...

    journal_title：European journal of medicinal chemistry

    pub_type： 杂志文章

    doi：10.1016/j.ejmech.2016.03.038

    authors： Velthuisen EJ,Johns BA,Temelkoff DP,Brown KW,Danehower SC

    更新日期：2016-07-19 00:00:00